[041] ESR: Catecholamines Flashcards
Compare between the importance of Catecholamine uptake and metabolism in terminating it’s actions
N.B.: Uptake is more important than metabolism in terminating the actions of catecholamines
Adrenaline and noradrenaline concentrations are controlled by……
post-ganglionic endocytosis
Polarity of Catecholamines ?
Catecholamines are hydrophilic and thus they interact with plasma membrane receptors
Effect of continuous exposure to stimulating ligand on G Protein Coupled Receptor ?
Desensitization = failure of signaling pathway to respond to stimulus despite continued presence of receptors at cell surface
….. adrenoceptors when activated, generally produce excitatory responses of smooth muscle
Alpha adrenoceptors
….. when activated, generally produce inhibitory responses of smooth muscle in which they are located
Beta receptors
Which Alpha Adrenoreceptors are pre/post synaptic ?
• alpha-1 receptors are mainly postsynaptic (on target organ cells)
• alpha-2 receptors are found mainly presynaptically (before the target cells) on sympathetic postganglionic nerve terminals
The major antihypertensive action of selective alpha-2 agonists such as clonidine, probably occurs as a result of …..
agonism of alpha-2 receptors in the CNS
Clonidine mechanism of action ?
• Clonidine treats high blood pressure by stimulating presynaptic alpha-2, decreasing presynaptic calcium levels, thus inhibiting the release of norepinephrine in the brainstem vasomotor center, decreasing sympathetic tone and peripheral vascular resistance, lowering blood pressure
Difference between Beta 1/2 and 3 Adrenoreceptors ?
• Beta-1produce cardiac positive chronotropic and inotropic responses and lipolysis
• Beta-2 receptors, when activated, produce bronchodilation, vasodilation, and uterine relaxation
• Beta-3 receptors produce lipolysis in adipose tissue
Selective Beta-2 agonists are useful in the treatment of……
asthma